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CRBN PROTAC® 14a

Cat. No. 7219 Submit a Review Datasheet / COA / SDS
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Description: Cereblon Degrader (PROTAC®)
Chemical Name: N1-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-N20-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,9,12,18-tetraoxaicosanediamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for CRBN PROTAC® 14a

CRBN PROTAC® 14a is a cereblon Degrader (PROTAC®). Comprises a ligand for Von Hippel Lindau (VHL) protein joined by a linker to a cereblon targeting ligand. Preferentially degrades cereblon (DC50 = 200 nM in HEK293 cells). Induces rapid and profound cereblon degradation (98% decrease after 8 h at 1 μM in HEK293 cells).

CRBN antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # NBP1-91810.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under licence from the University of Dundee

Technical Data for CRBN PROTAC® 14a

M. Wt 1061.26
Formula C53H72N8O13S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2358775-70-7
PubChem ID 138911387
InChI Key PEZCAXDTKNFUCR-CTMFSBKBSA-N
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCCCCOCCOCCCCCOCC(NCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)=O)O)=O)SC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CRBN PROTAC® 14a

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 106.13 100

Preparing Stock Solutions for CRBN PROTAC® 14a

The following data is based on the product molecular weight 1061.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.94 mL 4.71 mL 9.42 mL
5 mM 0.19 mL 0.94 mL 1.88 mL
10 mM 0.09 mL 0.47 mL 0.94 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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Product Datasheets for CRBN PROTAC® 14a

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for CRBN PROTAC® 14a

References are publications that support the biological activity of the product.

Girardini et al (2019) Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg.Med.Chem. 27 2466 PMID: 30826187

If you know of a relevant reference for CRBN PROTAC® 14a, please let us know.

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Citations for CRBN PROTAC® 14a

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia